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有机化学
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有机化学 ›› 2006, Vol. 26 ›› Issue (06): 808-812. 上一篇    下一篇

研究论文

3-芳烷氨基-6-氯哒嗪的合成及其除草活性

胡方中，张敏，刘斌，邹小毛，杨华铮*   

  1. (南开大学元素有机化学研究所 元素有机化学国家重点实验室 天津 300071)
  • 收稿日期:2005-07-07 修回日期:2005-12-08 发布日期:2006-05-31

Synthesis and Herbicidal Activity of 3-Arylalkylamino-6-chloropyridazines

HU Fang-Zhong,ZHANG Min,LIU Bin,ZOU Xiao-Mao,YANG Hua-Zheng*   

  1. (State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry,
    Nankai University, Tianjin 300071)
  • Received:2005-07-07 Revised:2005-12-08 Published:2006-05-31

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1846

被引次数

8 | 4

通过3,6-二氯哒嗪与(未)取代芳烷基胺在DMF/NaH或正丁醇体系缩合, 合成了13个3-芳甲(乙)氨基-6-氯哒嗪类化合物, 其中11个为新化合物, 它们的结构均经1H NMR, IR和元素分析确证. 初步的生物活性测试结果表明, 所合成的化合物对阔叶杂草有一定的抑制作用, 如化合物4f在施药量为10 µg•mL－1时对油菜的抑制率是76.42%. 讨论了其结构与除草活性的关系.

关键词: 除草活性, 构效关系, 3-芳烷氨基-6-氯哒嗪, 合成

A series of 3-arylalkylamino-6-chloropyridazines have been synthesized by the condensation of 3,6-dichloropyridazine with (un)substituted arylalkylamines in N,N-dimethylformamide (DMF) catalyzed by NaH at 120～130 ℃ or n-BuOH under reflux, and confirmed by 1H NMR, IR spectra and elemental analyses. Preliminary bioassay showed that some of them have certain herbicidal activity against broad leaf grasses, for example, at the dosage of 10 µg•mL－1, the inhibition percentage of compound 4f against Brassica napus reached 76.42%. Moreover, the structure-activity relationship was discussed.

Key words: herbicidal activity, structure-activity relationship, synthesis, 3-arylalkylamino-6-chloropyridazine